120417-13-2Relevant academic research and scientific papers
A library of spirooxindoles based on a stereoselective three-component coupling reaction
Lo, Michael M.-C.,Neumann, Christopher S.,Nagayama, Satoshi,Perlstein, Ethan O.,Schreiber, Stuart L.
, p. 16077 - 16086 (2004)
A collection of structurally complex and chemically diverse small molecules is a useful tool to explore cell circuitry. In this article, we report the split-pool synthesis of more than 3000 spirooxindoles on high capacity macrobeads. The key reaction to a
Synthesis of novel NHC–Rh complexes with anti-tumor activity against MCF-7 human breast cancer cells
He, Weiping,Li, Jie,Shi, Lu,Yang, Fan,Zhao, Xiong
, (2020/09/07)
A series of novel N-heterocyclic carbene rhodium complexes (NHC–Rh), containing benzimidazole framework, were prepared smoothly by a five-step route. Their structures were elucidated based on spectral techniques, including NMR and MS spectrometry. Along with several NHC–Rh complexes we prepared before, the compounds prepared herein were evaluated for their cytotoxicities against MCF human breast cancer cells and several of them showed strong activities with IC50 values ranging from 0.38 to 1.18μM, which were better than the positive control paclitaxel.
COMPLEMENT MODULATORS AND RELATED METHODS
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Paragraph 0391, (2020/10/20)
The present disclosure presents compounds and compositions that interact with complement components. Some compounds inhibit complement activity. Included are small molecule compounds and compositions that function as C5 inhibitor compounds. Methods for inhibiting complement activity and methods of treating complement-related indications with the C5 inhibitor compounds and compositions are provided.
Direct Conversion of N-Alkylamines to N-Propargylamines through C-H Activation Promoted by Lewis Acid/Organocopper Catalysis: Application to Late-Stage Functionalization of Bioactive Molecules
Chan, Jessica Z.,Yesilcimen, Ahmet,Cao, Min,Zhang, Yuyang,Zhang, Bochao,Wasa, Masayuki
supporting information, p. 16493 - 16505 (2020/10/26)
An efficient catalytic method to convert an α-C-H bond of N-alkylamines into an α-C-alkynyl bond was developed. In the past, such transformations were carried out under oxidative conditions, and the enantioselective variants were confined to tetrahydroisoquinoline derivatives. Here, we disclose a method for the union of N-alkylamines and trimethylsilyl alkynes, without the presence of an external oxidant and promoted through cooperative actions of two Lewis acids, B(C6F5)3 and a Cu-based complex. A variety of propargylamines can be synthesized in high diastereo-and enantioselectivity. The utility of the approach is demonstrated by the late-stage site-selective modification of bioactive amines. Kinetic investigations that shed light on various mechanistic nuances of the catalytic process are presented.
FUSED TRIAZOLE AGONISTS OF THE APJ RECEPTOR
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Paragraph 0291-0292, (2019/05/22)
Compounds of Formula I, pharmaceutically acceptable salts thereof, tautomers thereof, pharmaceutically acceptable salts of the tautomers, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula (I) have the following structure: where the definitions of the variables are provided herein.
Chirality n-heterocyclic carbine precursor compound with benzoglioxaline frameworks and preparation method and application thereof
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Paragraph 0073; 0074; 0076; 0077, (2018/09/14)
The invention discloses chirality n-heterocyclic carbine precursor compound with benzoglioxaline frameworks and a preparation method and application thereof. Five steps of reaction can simply and effectively compound a series of chirality benzoglioxaline
BENZOXAZEPIN OXAZOLIDINONE COMPOUNDS AND METHODS OF USE
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Paragraph 0195-0196, (2017/01/23)
Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure: or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.
Efficient Routes to a Diverse Array of Amino Alcohol-Derived Chiral Fragments
Haftchenary, Sina,Nelson, Shawn D.,Furst, Laura,Dandapani, Sivaraman,Ferrara, Steven J.,Bo?kovi?, ?arko V.,Figueroa Lazú, Samuel,Guerrero, Adrian M.,Serrano, Juan C.,Crews, Demarcus K.,Brackeen, Cristina,Mowat, Jeffrey,Brumby, Thomas,Bauser, Marcus,Schreiber, Stuart L.,Phillips, Andrew J.
supporting information, p. 569 - 574 (2016/10/06)
Efficient syntheses of chiral fragments derived from chiral amino alcohols are described. Several unique scaffolds were readily accessed in 1-5 synthetic steps leading to 45 chiral fragments, including oxazolidinones, morpholinones, lactams, and sultams. These fragments have molecular weights ranging from 100 to 255 Da and are soluble in water (0.085 to >15 mM).
Discovery of a selective TRPM8 antagonist with clinical efficacy in cold-related pain
Andrews, Mark D.,Af Forselles, Kerry,Beaumont, Kevin,Galan, Sébastien R. G.,Glossop, Paul A.,Grenie, Mathilde,Jessiman, Alan,Kenyon, Amy S.,Lunn, Graham,Maw, Graham,Owen, Robert M.,Pryde, David C.,Roberts, Dannielle,Tran, Thien Duc
supporting information, p. 419 - 424 (2015/04/27)
The transient receptor potential (TRP) family of ion channels comprises nonselective cation channels that respond to a wide range of chemical and thermal stimuli. TRPM8, a member of the melastatin subfamily, is activated by cold temperatures (28 °C), and antagonists of this channel have the potential to treat cold induced allodynia and hyperalgesia. However, TRPM8 has also been implicated in mammalian thermoregulation and antagonists have the potential to induce hypothermia in patients. We report herein the identification and optimization of a series of TRPM8 antagonists that ultimately led to the discovery of PF-05105679. The clinical finding with this compound will be discussed, including both efficacy and its ability to affect thermoregulation processes in humans.
Asymmetric induction in 8π electrocyclizations. Design of a removable chiral auxiliary
Kim, Keunsoo,Lauher, Joseph W.,Parker, Kathlyn A.
supporting information; experimental part, p. 138 - 141 (2012/03/08)
The pseudo C2 symmetric trans diphenyl oxazoline group acts as an effective chiral auxiliary in the 8π, 6π tandem electrocyclization of a substituted tetraene 1-carboxylic acid. Assignment of absolute stereochemistry to the [4.2.0] bicyclooctad
